title: cis-Dichloroplatinum(II) complexes tethered to dibenzo[c,h][1,6]naphthyridin-6-ones: synthesis and cytotoxicity in human cancer cell lines in vitro.
abstract: A novel family of cisplatin-type complexes tethered to dibenzo[c,h][1,6]naphthyridin-6-one topoisomerase inhibitor via a polymethylene chain and their nonplatinated counterparts were prepared. Their potential cytotoxicity was assessed in three human colorectal cancer cell lines HCT 116, SW480 and HT-29 and compared to the reference molecules cisplatin and oxaliplatin. Platinated compounds were poorly active whilst nonplatinated dibenzo[c,h][1,6]naphthyridin-6-one moieties exhibited higher cytotoxic properties than cisplatin and oxaliplatin whatever the length of the polymethylene chain; molecules containing the tri- and hexamethylene chain length were the most cytotoxic.
authors.affiliation: INSERM UMR U866 "Lipides/Nutrition/Cancer", Université de Bourgogne, UFR Médecine, 7 bd Jeanne d'Arc, BP 89700, 21079 Dijon Cedex, France. Electronic address: nicolas.desbois@u-bourgogne.fr.
authors.forename: Nicolas
authors.initials: N
authors.lastname: Desbois
authors.forename: David
authors.initials: D
authors.lastname: Pertuit
authors.forename: Johnny
authors.initials: J
authors.lastname: Moretto
authors.forename: Claire
authors.initials: C
authors.lastname: Cachia
authors.forename: Bruno
authors.initials: B
authors.lastname: Chauffert
authors.forename: Florence
authors.initials: F
authors.lastname: Bouyer
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D019073:HT29 Cells; D006801:Humans; D015394:Molecular Structure; D009287:Naphthyridines / Q000737:chemistry*; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009287:Naphthyridines; D009944:Organoplatinum Compounds
keywords: 5H-Dibenzo[c,h][1,6]naphthyridin-6-one; Cisplatin; Colorectal cancer cell; Cytotoxicity; Topoisomerase I targeting agents